Genard P, Palem-Vliers M
J Steroid Biochem. 1985 Nov;23(5A):673-5. doi: 10.1016/0022-4731(85)90021-4.
Deoxycorticosterone acetate (DOCA) and 9 alpha-fluorocortisol acetate (9 alpha-F-Cac) can be modified by the introduction of a double bond at carbons 6 and 7 (6-dehydro-derivatives). Such a modification markedly changes the effect of the steroids on urinary excretion of Na+ and K+. Since 6-7 reduction of DOCA and 9 alpha-F-Cac substantially reduces affinity for Type II receptors but not Type I receptors, 6-dehydro-derivatives will thus bind preferentially to receptors influencing the retention of sodium (the "mineralocorticoid" or Type I receptor), and compete with mineralocorticoids for such receptors. We interpret the increase in both natriuresis and kaliuresis when mineralocorticoids and their dehydro-derivatives are administered together as evidence for a Type II receptor mediation of these ion fluxes.
醋酸脱氧皮质酮(DOCA)和醋酸9α-氟皮质醇(9α-F-Cac)可通过在碳6和碳7处引入双键(6-脱氢衍生物)进行修饰。这种修饰显著改变了类固醇对尿中Na⁺和K⁺排泄的影响。由于DOCA和9α-F-Cac的6-7还原会大幅降低对II型受体的亲和力,但对I型受体无影响,因此6-脱氢衍生物将优先与影响钠潴留的受体(“盐皮质激素”或I型受体)结合,并与盐皮质激素竞争此类受体。我们将盐皮质激素及其脱氢衍生物共同给药时钠利尿和钾利尿均增加的现象解释为这些离子通量由II型受体介导的证据。